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2g |
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5g |
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10g |
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25g |
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50g |
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100g |
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200g |
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Other Sizes |
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Purity: ≥98%
Lidocaine hydrochloride monohydrate (also known as Alphacaine; Lignocaine) is a potent and selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Lidocaine is a local anesthetic and cardiac depressant used as an antiarrhythmia agent. Originally developed as a local anesthetic, it has properties as a class IB antiarrhythmic, a long-acting membrane stabilizing agent used against ventricular arrhythmia. Its actions are more intense and its effects more prolonged than those of procaine but its duration of action is shorter than that of bupivacine or prilocaine.
ln Vitro |
Cell growth is dramatically reduced by lignocaine (10 nM; 48 hours) [2]. Cell viability is inhibited by lidocaine (1-10 nM; 24-72 hours); the maximum inhibitory effect is obtained at a dose of 10 nM and a treatment duration of 48 hours [2]. The rate of apoptosis is markedly increased by lidocaine (10 nM; 48 hours) [2]. Lidocaine (10 nM; 48 hours) dramatically increases the expression of p21 and downregulates Cyclin D1 [2].
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ln Vivo |
In rats, lidocaine (lidocaine) produces a completely reversible block of the tail nerve. Compared to thermal nociceptive blockade, mechanical nociceptive blockade, which is generated by lidocaine, has a slower onset and a quicker recovery [3].
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Cell Assay |
Cell proliferation experiment [2]
Cell Types: human gastric cancer cell line MKN45 Tested Concentrations: 10 nM Incubation Duration: 48 hrs (hours) Experimental Results: Cell proliferation diminished Dramatically. Cell viability assay [2] Cell Types: human gastric cancer cell line MKN45 Tested Concentrations: 1, 5 and 10 nM Incubation Duration: 24, 48, 72 hrs (hours) Experimental Results: Inhibition of MKN45 cell viability. Cell apoptosis analysis [2] Cell Types: Human gastric cancer cell line MKN45 Tested Concentrations: 10 nM Incubation Duration: 48 hrs (hours) Experimental Results: The cell apoptosis rate increased Dramatically. Western Blot Analysis [2] Cell Types: human gastric cancer cell line MKN45 Tested Concentrations: 10 nM Incubation Duration: 48 hrs (hours) Experimental Results: Cyclin D1 expression was Dramatically down-regulated, and p21 expression was Dramatically up-regulated. |
References |
[1]. Cummins TR, et al. Setting up for the block: the mechanism underlying lidocaine's use-dependent inhibition of sodium channels. J Physiol. 2007 Jul 1;582(Pt 1):11.
[2]. Sui H, et al. Lidocaine inhibits growth, migration and invasion of gastric carcinoma cells by up-regulation of miR-145. BMC Cancer. 2019 Mar 15;19(1):233. [3]. Li Z, et al. Evaluation of the antinociceptive effects of lidocaine and bupivacaine on the tail nerves of healthy rats. Basic Clin Pharmacol Toxicol. 2013 Jul;113(1):31-6. |
Molecular Formula |
C14H25CLN2O2
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Molecular Weight |
288.816
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CAS # |
6108-05-0
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Related CAS # |
Lidocaine;137-58-6
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SMILES |
CCN(CC)CC(=O)NC1=C(C=CC=C1C)C.Cl
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InChi Code |
InChI=1S/C14H22N2O.ClH/c1-5-16(6-2)10-13(17)15-14-11(3)8-7-9-12(14)4;/h7-9H, 5-6,10H2,1-4H3,(H,15,17);1H;
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Chemical Name |
2-(diethylamino)-N-(2,6-dimethylphenyl)acetamide;hydrate;hydrochloride;
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Synonyms |
Lidocaine Hydrochloride; LIDOCAINE HCL; Lidothesin; Lignocaine hydrochloride; Xyloneural; Xylocitin;
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.4624 mL | 17.3118 mL | 34.6236 mL | |
5 mM | 0.6925 mL | 3.4624 mL | 6.9247 mL | |
10 mM | 0.3462 mL | 1.7312 mL | 3.4624 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.